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    1. Cell Biology
    2. Cancer Biology

    A kinase-independent function of AKT promotes cancer cell survival

    Igor Vivanco et al.
    The oncogenic potential of the serine threonine kinase AKT is not exclusively dependent on catalytic activity, but also involves the non-catalytic function of the pleckstrin homology domain.
    1. Cancer Biology

    MARCH5 mediates NOXA-dependent MCL1 degradation driven by kinase inhibitors and integrated stress response activation

    Seiji Arai et al.
    MARCH5 mediates a pathway driving MCL1 degradation in response to cellular stress, which sensitizes to BH3 mimetic drugs targeting BCLXL and provides a broadly effective therapeutic strategy for solid tumors.
    1. Cell Biology

    Probing the catalytic functions of Bub1 kinase using the small molecule inhibitors BAY-320 and BAY-524

    Anna P Baron et al.
    Chemical inhibition of Bub1 shows that the catalytic activity is not required for normal mitotic progression, but it makes chromosome segregation and cell proliferation more sensitive to the effects of the anti-cancer drug Paclitaxel.
    1. Biochemistry and Chemical Biology
    2. Cell Biology

    Hypothemycin, a fungal natural product, identifies therapeutic targets in Trypanosoma brucei

    Mari Nishino et al.
    Hypothemycin, which inhibits a number of protein kinases, kills the T. brucei parasites that cause sleeping sickness and reveals new therapeutic targets for the disorder.
    1. Biochemistry and Chemical Biology
    2. Cell Biology

    Subcellular drug targeting illuminates local kinase action

    Paula J Bucko et al.
    Genetically-encoded platforms direct kinase inhibitor drugs to organelles to reveal new dimensions of local kinase signaling.
    1. Biochemistry and Chemical Biology
    2. Structural Biology and Molecular Biophysics

    Flexible linkers in CaMKII control the balance between activating and inhibitory autophosphorylation

    Moitrayee Bhattacharyya et al.
    Differences in the flexible linkers connecting the kinase domain to an oligomeric hub modulate CaMKII activity by changing the balance between activating and inhibitory autophosphorylation.
    1. Neuroscience

    The switch-like expression of heme-regulated kinase 1 mediates neuronal proteostasis following proteasome inhibition

    Beatriz Alvarez-Castelao et al.
    In neurons, inhibition of the proteasome results in feedback inhibition of protein synthesis, mediated by heme-regulated kinase 1, which is optimized to act as both a sensor and an effector.
    1. Cell Biology

    An extensive program of periodic alternative splicing linked to cell cycle progression

    Daniel Dominguez et al.
    Extensive periodic regulation of alternative splicing during the cell cycle in genes is linked to cell cycle functions, and involves an auto-inhibitory mechanism that uses the protein kinase CLK1.
    1. Biochemistry and Chemical Biology
    2. Cancer Biology

    Overcoming myelosuppression due to synthetic lethal toxicity for FLT3-targeted acute myeloid leukemia therapy

    Alexander A Warkentin et al.
    Anti-targets are proteins that cause problems when inhibited along with an intended target and our novel chemical strategy affords unprecedented selectivity in the context of FLT3 vs. KIT inhibition for treatment of a devastating blood cancer.
    1. Cancer Biology

    FGF2-FGFR1 signaling regulates release of Leukemia-Protective exosomes from bone marrow stromal cells

    Nathalie Javidi-Sharifi et al.
    Inhibition of FGF2-FGFR1 signaling in bone marrow stroma attenuates secretion of FGF2-laden exosomes and subsequent protection of leukemia cells.